专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US06451823B1 Use of substituted N-phenoxy-N-phenyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译：使用取代的N-苯氧基-N-苯基氨基醇化合物抑制胆固醇酯转移蛋白活性
公开(公告)号：US06451823B1
公开(公告)日：2002-09-17
申请号：US09990645
申请日：2001-11-14
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： C07C23300
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols. A preferred specific N-phenoxy-N-phenyl aminoalcohol is the compound:
摘要翻译：本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。优选的叔杂烷基胺化合物是取代的N-苯氧基-N-苯基氨基醇。优选的特定N-苯氧基-N-苯基氨基醇是化合物：

42. 发明授权

US06358993B1 Pharmaceutically active nitrogen ring compounds and methods of use thereof 失效
标题翻译：药用活性氮环化合物及其使用方法
公开(公告)号：US06358993B1
公开(公告)日：2002-03-19
申请号：US09425582
申请日：1999-10-22
申请人： N. Laxma Reddy , Michael Maillard , David Berlove , Sharad Magar , Graham J. Durant
发明人： N. Laxma Reddy , Michael Maillard , David Berlove , Sharad Magar , Graham J. Durant
IPC分类号： A61K31405
CPC分类号： C07D209/08 , C07D209/90 , C07D209/92 , C07D215/08 , C07D215/12 , C07D221/12 , C07D223/22 , C07D225/08 , C07D231/12 , C07D233/56 , C07D249/08 , C07D265/36 , C07D277/62 , C07D279/16 , C07D281/10 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
摘要翻译：本发明涉及药学上可接受的化合物，包括某些取代的二氢吲哚基及其衍生物，1,2,3,4-四氢喹啉基及其衍生物，1,2,3,4-四氢异喹啉基，苯并[cd] 二氢吩芬丁基化合物，以及使用或包含一种或多种这样的化合物的治疗方法和药物组合物。本发明的化合物特别可用于治疗或预防神经损伤和神经变性疾病。

43. 发明授权

US5990104A Polycyclic alcaloid-derivatives as NMDA-receptor antagonists 失效
标题翻译：多环类别衍生物作为NMDA-受体拮抗剂
公开(公告)号：US5990104A
公开(公告)日：1999-11-23
申请号：US981935
申请日：1998-03-25
申请人： John Dimaio , Dilip M. Dixit
发明人： John Dimaio , Dilip M. Dixit
IPC分类号： A61K31/135 , A61K31/335 , A61K31/38 , A61P25/00 , A61P25/08 , A61P43/00 , C07C215/44 , C07D221/22 , C07D225/08 , C07D313/00 , C07D313/20 , C07D337/16 , A61K31/00
CPC分类号： C07C215/44 , C07D225/08 , C07D313/20 , C07D337/16
摘要： Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor. ##STR1##
摘要翻译： PCT No.CPC / CA96 / 00468 Sec。 371日期：1998年3月25日 102（e）1998年3月25日PCT PCT 1996年7月12日PCT公布。公开号WO97 / 03929 日期：1997年2月6日式（I）的多环生物碱，其中R 1为H，C 1-6烷基或任选被极性基团取代的C 6-12芳基; R2和R3独立地是H，OH，C1-6烷基，-C（NH）-NH2，带正电荷的基团或任选被NH 2，OH，C 1-6烷基或卤素取代的C 7-13芳烷基; 或R 2和R 3一起形成任选地加入杂原子的5至6元环; R4是H，C1-6烷基，OR6，SR6或N（R6）2，其中每个R6独立地是H，C1-3烷基; X ix O，S，SO，SO 2或N-R 5，其中每个R 5独立地为H，C 1-6烷基或任选被一个或多个杂原子间断的C 7-13芳烷基; n为0〜2的整数; m是0-3的整数。这些化合物在离子型NMDA（N-甲基 - （D） - 天冬氨酸）受体上起拮抗剂的作用。

44. 发明授权

US5760031A Tricyclic benzazepine vasopressin antagonists 失效
公开(公告)号：US5760031A
公开(公告)日：1998-06-02
申请号：US637911
申请日：1996-04-25
申请人： Jay Donald Albright , Marvin Fred Reich
发明人： Jay Donald Albright , Marvin Fred Reich
IPC分类号： C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/55 , C07D498/02
CPC分类号： C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

45. 发明授权

US5686466A Tricyclic condensed heterocyclic compounds their production and use 失效
标题翻译：三环稠合杂环化合物的生产和使用
公开(公告)号：US5686466A
公开(公告)日：1997-11-11
申请号：US618796
申请日：1996-03-20
申请人： Giichi Goto , Yuji Ishihara , Keisuke Hirai
发明人： Giichi Goto , Yuji Ishihara , Keisuke Hirai
IPC分类号： C07D209/86 , C07D209/90 , C07D211/26 , C07D223/18 , C07D223/22 , C07D225/08 , C07D267/18 , C07D307/91 , C07D401/06 , C07D413/06 , C07D471/06 , C07D487/06
CPC分类号： C07D307/91 , C07D209/86 , C07D209/90 , C07D211/26 , C07D223/18 , C07D223/22 , C07D225/08 , C07D267/18 , C07D401/06 , C07D413/06 , C07D471/06 , C07D487/06
摘要： A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
摘要翻译：一种下式的新化合物：其中Ar表示任选取代的三环稠合苯环，其包含至少一个杂环作为组分环; n表示2〜10的整数， R1表示H或任选取代的烃基，其可以在重复n时彼此不同; Y表示任选取代的4-哌啶基，1-哌嗪基或4-苄基-1-哌啶基或其盐，其抑制优异的胆碱酯酶抑制活性和单胺再摄取抑制活性，因此可用作治疗和/或预防药物老年性痴呆。

46. 发明授权

US5512563A Tricyclic benzazepine vasopressin antagonists 失效
公开(公告)号：US5512563A
公开(公告)日：1996-04-30
申请号：US254823
申请日：1994-06-13
申请人： Jay D. Albright , Fuk-Wah Sum , Xuemei Du
发明人： Jay D. Albright , Fuk-Wah Sum , Xuemei Du
IPC分类号： A61K31/395 , A61K31/435 , A61K31/473 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61P1/16 , A61P9/04 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P43/00 , C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D223/28 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D245/04 , C07D267/16 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/00 , C07D281/14 , C07D281/16 , C07D285/00 , C07D285/38 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D401/12 , C07D221/12 , C07D221/18 , C07D223/18 , C07D223/20 , C07D223/22 , C07D225/00 , C07D225/08 , C07D243/18 , C07D243/38 , C07D267/18 , C07D267/20 , C07D279/30 , C07D281/16 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

47. 发明授权

US4649196A Process for the manufacture of racemic (R,R; S,S) asocainol 失效
标题翻译：用于制备外消旋（R，R; S，S）asocainol的方法
公开(公告)号：US4649196A
公开(公告)日：1987-03-10
申请号：US730124
申请日：1985-05-03
申请人： Wolfgang Herrmann , Gerhard Satzinger
发明人： Wolfgang Herrmann , Gerhard Satzinger
IPC分类号： A61K31/395 , A61P9/06 , C07D225/08
CPC分类号： C07D225/08
摘要： A process for the preparation of racemic asocainol in the (R,R; S,S)-form and (-)-asocainol in the (S,S)-form as well as the pharmacologically compatible salts thereof is herein described on the basis of a thermal rearrangement of the inactive (R,S)-diastereomer to the (S,S)-form.Racemic (.+-.)-asocainol and the (-)-enantiomer are potent antiarrhythmic agents and local anesthetics.
摘要翻译：在（S，S）形式的（R，R; S，S）形式和（ - ） - 焦氨醇中制备外消旋asocainol以及其药理学上相容的盐的方法在此基于的非活性（R，S） - 非对映体与（S，S） - 形式的热重排。外消旋（+/-） - asocainol和（ - ） - 对映异构体是有效的抗心律失常药和局部麻醉药。

48. 发明授权

US3950344A Non-phenol oxidative coupling 失效
标题翻译：非酚类氧化偶联
公开(公告)号：US3950344A
公开(公告)日：1976-04-13
申请号：US396811
申请日：1973-09-13
申请人： Solomon Morris Kupchan , Andris J. Liepa
发明人： Solomon Morris Kupchan , Andris J. Liepa
IPC分类号： C07D209/96 , C07D217/20 , C07D221/18 , C07D225/08 , C07D215/12 , C07D221/26
CPC分类号： C07D221/18 , C07D209/96 , C07D217/20 , C07D225/08
摘要： Oxidative coupling of non-phenolic compounds is attained by subjecting said non-phenolic compound to oxidizing conditions in contact with an oxidant selected from the group of VOF.sub.3, MoOCl.sub.4, Pb.sub.3 O.sub.4, Tl(CF.sub.3 COO).sub.3, CrO.sub.3, MnO.sub.2, Co(OH).sub.3, Ce(SO.sub.4).sub.2, and Ce(NH.sub.4).sub.2 (NO.sub.3).sub.6.

49. 发明授权

US3514444A Dibenz(b,f)azocines-6-ones 失效
标题翻译： DIBENZ（B，F）AZOCINES-6-ONES
公开(公告)号：US3514444A
公开(公告)日：1970-05-26
申请号：US3514444D
申请日：1968-11-29
申请人： SQUIBB & SONS INC
发明人： YALE HARRY LOUIS , SOWINSKI FRANCIS A
IPC分类号： C07D225/08 , C07D41/00
CPC分类号： C07D225/08

50. 发明公开

US20240300900A1 HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES AND METAL-FREE CLICK REACTIONS WITH THESE HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES 审中-公开
公开(公告)号：US20240300900A1
公开(公告)日：2024-09-12
申请号：US18660802
申请日：2024-05-10
申请人： Roche Diagnostics Operations, Inc.
发明人： Frank Bergmann , Dieter Heindl , Nils Winter
IPC分类号： C07D225/08 , A61K47/54 , A61K49/00 , A61K51/04
CPC分类号： C07D225/08 , A61K47/545 , A61K49/0052 , A61K51/044
摘要： The invention relates in a first aspect to an azadibenzocyclooctyne derivative according to formula (I) or a salt thereof having specific substituents at the benzo rings of the DIBAC structure and having specific substituents connected to the nitrogen atom of the DIBAC structure. A second aspect of the invention is directed to a conjugate of formula (II), wherein a substituent R6 is connected to the N atom of the 8 membered ring of the DIBAC structure via a linker structure —C(═O)-[L]n-Z—. A third aspect of the invention relates to a method for the modification of a target molecule, wherein a conjugate according to the second aspect is reacted with a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group. In a fourth aspect, the invention is directed to the use of the conjugate according to the second aspect for bioorthogonal labeling and/or modification of a target molecule. A fifth aspect of the invention relates to a modified target molecule comprising the reaction product of a conjugate according to the second aspect and a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group, obtained or obtainable from the method of the third aspect. In a sixth aspect, the invention is related to a kit comprising a modified target molecule according to the fifth aspect as detector reagent and a suitable capture reagent.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式